| Company Name: |
TargetMol |
| Tel: |
400-821-0310 15002144251 |
| Email: |
xuexiang.shao@tsbiochem.com |
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| Product Name: | MU1210 | | Synonyms: | MU1210;Furo[3,2-b]pyridine, 5-(1-methyl-1H-pyrazol-4-yl)-3-[3-(4-pyridinyl)phenyl]- | | CAS: | 2275601-87-9 | | MF: | C22H16N4O | | MW: | 352.39 | | EINECS: | | | Product Categories: | | | Mol File: | 2275601-87-9.mol |  |
| | MU1210 Chemical Properties |
| Boiling point | 589.0±50.0 °C(Predicted) | | density | 1.28±0.1 g/cm3(Predicted) | | storage temp. | -20°C | | solubility | DMSO: 2mg/mL, clear | | pka | 4.96±0.26(Predicted) | | form | powder | | color | white to beige | | InChI | 1S/C22H16N4O/c1-26-13-18(12-24-26)20-5-6-21-22(25-20)19(14-27-21)17-4-2-3-16(11-17)15-7-9-23-10-8-15/h2-14H,1H3 | | InChIKey | HEAGNKNMQVIVMM-UHFFFAOYSA-N | | SMILES | CN(N=C1)C=C1C2=CC=C3C(C(C4=CC=CC(C5=CC=NC=C5)=C4)=CO3)=N2 |
| WGK Germany | WGK 3 | | Storage Class | 11 - Combustible Solids |
| | MU1210 Usage And Synthesis |
| Uses | MU1210 (compound 12f) is an inhibitor of CDC-like kinases Clk1, Clk2, and Clk4 (with IC50 values of 8, 20, and 12 nM respectively), with IC50 for HIPK1 and DYRK2 are 187 and 1309 nM. MU1210 also has favorable pharmacokinetic characteristics (in mice, 10 mg/kg, intraperitoneal injection: Cmax=1.24 μM, T1/2=58 minutes; no acute toxicity observed)[1]. | | Biological Activity | MU1210 is a potent and selective inhibitor against cdc-like kinase (cdc2-like kinase) CLK1, CLK2, CLK4 (CLK1/2/4 IC50 = 8/20/12 nM; CLK1/2/4 Ki = 84/91/23 nM by NanoBRET) and HIPK2 (IC50 = 29 nM) with good selectivity over HIPK1/3 (IC50 = 187/159 nM), DYRK1a/1b/2 (IC50 = 213/956/1309 nM), CLK3 (IC50 >3 μM) and 194 other kinases. MU1210 enhances alternative spliced MDM4-S mRNA (10 μM, 24 h) and exhibits antiproliferation activity in MCF7 cultures (IC50 in 72 h = 1.1 μM). Unlike most ATP site-targeting kinase inhibitors, X-ray crystallography shows th at MU1210 is anchored to the back pocket instead of the hinge region of CLK1. MU140 serves as a negative control. | | IC 50 | CLK1: 8 nM (IC50); CLK2: 20 nM (IC50); CLK4: 12 nM (IC50); HIPK1: 187 nM (IC50); DYRK2: 1309 nM (IC50) | | References | [1] Václav Němec, et al. Furo[3,2-b]pyridine: A Privileged Scaffold for Highly Selective Kinase Inhibitors and Effective Modulators of the Hedgehog Pathway. Angew Chem Int Ed Engl. 2019 Jan 21;58(4):1062-1066. DOI:10.1002/anie.201810312 |
| | MU1210 Preparation Products And Raw materials |
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